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Nrf2 Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
E1141 KI696 KI696 is a potent and selective inhibitor of KEAP1/NRF2 interaction. This compound induces the expression of each of the Nqo1, Ho-1, Txnrd1, Srxn1, Gsta3, Gclc genes in a dose-dependent manner.
Clin Mol Hepatol, 2025, 10.3350/cmh.2024.0948
Chin Med J (Engl), 2025, 138(13):1607-1620
Redox Biol, 2024, 72:103137
S9723 CDDO-Im (RTA-403) An activator of nuclear factor erythroid 2–related factor 2 (Nrf2) and peroxisome proliferator-activated receptor (PPAR), CDDO-Im (RTA-403) binds to PPARα and PPARγ with Ki of 232 nM and 344 nM, respectively. It inhibits inflammatory response and tumor growth in vivo.
Ecotoxicol Environ Saf, 2022, 241:113754
Int J Mol Sci, 2022, 23(19)11715
S3168 cis-Resveratrol cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively.
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
S3808 Mangiferin Mangiferin (Alpizarin, Chinomin, Hedysarid) is a bioactive compound that demonstrates many health perspectives and has been used to prepare medicinal and food supplements. This compound is a Nrf2 activator. It suppresses nuclear translocation of the NF-κB subunits p65 and p50.
Front Pharmacol, 2022, 13:1028932
E0441 NK-252 NK-252 is an activator of Nrf2 and interacts with the Nrf2-binding site of Keap1.
E1339 HPPE HPPE is a specific nonelectrophilic and physiological Bach1 inhibitor via heme-binding sites of Bach1 protein, derepresses Bach1-mediated repression.
E1220 CBR-470-1 CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). This compound is also a non-covalent Nrf2 activator. It protects SH-SY5Y neuronal cells against MPP+-induced cytotoxicity through activation of the Keap1-Nrf2 cascade.
E3419 Ganoderma lucidum Extract Ganoderma lucidum Extract is extracted from Ganoderma lucidum, which can regulate Nrf2 and Nrf2-related proteins.
E3427 Uniflower swisscentaury root Extract Uniflower swisscentaury root Extract is extracted from the root of Rhaponticum uniflorum (L.) DC., which can alleviate inflammatory responses via the Nrf2/HO-1 signaling pathway.
E0023 5,7-Dihydroxychromone

5,7-Dihydroxychromone (DHC), a natural antioxidant extracted from plants, is a potent activator of Nrf2/ARE signal. This compound also is a potent activator of PPARγ and LXRα. It may contributes to regulate blood glucose levels and shows anti-diabetic property.
E1973 R16 R16(NSC29869, Nrf2-IN-3) is an inhibitor of NRF2 (nuclear factor erythroid 2-related factor 2) that selectively binds KEAP1 mutants and restores their NRF2-inhibitory function by repairing the disrupted KEAP1/NRF2 interactions. It significantly enhances the sensitivity of KEAP1-mutated tumor cells to cisplatin and gefitinib.
E0129 Oxysophocarpine Oxysophocarpine (OSC) is an alkaloid extracted from Sophora alopecuroides. This compound inhibits the growth and metastasis of oral squamous cell carcinoma (OSCC) by targeting the Nrf2/HO-1 axis. It protects cells against apoptosis and inflammatory responses and compromised miR-155 activity by attenuating MAPK and NF-κB pathways.
E4007 L-Sulforaphane L-Sulforaphane ((R)-Sulforaphane) is a highly potent inducer of the Keap1/Nrf2/ARE pathway. It is a more potent inducer of the carcinogen-detoxifying enzyme systems in rat liver and lung than the S-isomer.
S1848 Curcumin Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase（IC50~25 μM）and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.
J Biol Chem, 2025, 301(7):110305
Mol Pain, 2025, 21:17448069251323668
BMC Immunol, 2025, 26(1):67
Verified customer review of Curcumin
S3275 Senkyunolide I Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. This compound up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. It also promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.
Blood Sci, 2025, 7(3):e00246
iScience, 2024, 27(7):110367
World J Emerg Med, 2024, 15(3):206-213
S5144 Neferine Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. It induces apoptosis in renal cancer cells. This compound prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. It strongly inhibits NF-κB activation. It possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.
J Cosmet Dermatol, 2024, 10.1111/jocd.16587
Bone Res, 2022, 10(1):27
Cell Death Dis, 2022, 13(11):1000
S3784 Obacunone (AI3-37934) Obacunone (AI3-37934, CCRIS 8657), a natural compound present in citrus fruits, has been demonstrated for various biological activities including anti-cancer and anti-inflammatory properties. This compound significantly inhibits aromatase activity in an in vitro enzyme assay with an IC50 value of 28.04 μM; it is also a novel activator of Nrf2.
Int J Mol Sci, 2023, 24(14)11484
University of Valencia, 2023,
Cell Mol Biol Lett, 2022, 27(1):29
S3301 Cynarin Cynarin (Cynarine) is an artichoke phytochemical that possesses a variety of pharmacological features including free-radical scavenging, antioxidant, antihistamic and antiviral activities. This compound blocks the interaction between the CD28 of T-cell receptor and CD80 of antigen presenting cells. It triggers Nrf2 nuclear translocation, restores the balance of glutathione (GSH) and reactive oxygen species (ROS), and inhibits mitochondrial depolarization.
Int J Mol Med, 2025, 56(6)206
S3205 Perillaldehyde Perillaldehyde (Perilladehyde, Perillal, PAE, PA), the main component of Perilla frutescens (a traditional medicinal antioxidant herb), inhibits BaP-induced AHR activation and ROS production, inhibits BaP/AHR-mediated release of the CCL2 chemokine, and activats the NRF2/HO1 antioxidant pathway.
Front Cell Dev Biol, 2025, 13:1598520
E1281 Dimethyl itaconate Dimethyl itaconate can reprogram neurotoxic to neuroprotective primary astrocytes through the regulation of LPS-induced Nod-like receptor protein 3 (NLRP3) inflammasome and nuclear factor 2/heme oxygenase-1 (NRF2/HO-1) pathways.
E0526 sappanone A Sappanone A, a homoisoflavanone isolated from the heartwood of Caesalpinia sappan (Leguminosae), induces HO-1 expression by activating Nrf2 through the p38 MAPK pathway, suppresses LPS-induced NF-κB activation by suppressing the phosphorylation of RelA/p65 at Ser536, exerting its anti-inflammatory effect.
S4712 Diethylmaleate Diethylmaleate (Diethyl ester, Maleic acid diethyl ester) is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NF-κB.